Miransertib HCl

Biorbyt

Miransertib HCl [1313883-00-9]

10

1313883-00-9

Research Use Only

C27H25CLN6

468.9806039

Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

Cl.NC1(C2C=CC(=CC=2)N2C(C3=CC=CN=C3N)=NC3C=CC(C4C=CC=CC=4)=NC2=3)CCC1

12352200